Deoxypodophyllotoxin (DPT) is a compound extracted and purified from the traditional Chinese medicine Sinopodophyllum emodi (Wall.). It has been reported as early as 1990's that DPT has an in vitro inhibition effects on the cell lines of P-388 leukemia, human lung cancer A-549 and colon cancer HT-29 (Arch Pharm (Weinheim). 1994 March; 327 (3): 157˜9. Planta Med. 1993 June; 59 (3): 246˜9), but the studies only focus on the experiments on its in vitro activities. Experiments on in vivo activities have not been reported for more than ten years, which can be mainly attributed to that this compound is insoluble in water and can not be used to produce the preparations for intravenous injection. A series of glycoside derivatives were synthesized by using the hydroxyl group of position 4 in Podophyllotoxin in the 1970's, wherein the well known Etopside and Teniposide have been successfully applied to clinical practices. However, hydroxyl group is absent at the position 4 in DPT. Thus DPT can not be used to prepare glycoside derivative. It has become a key project for scientists that how to use DPT prepare injections thereof to validate its in vivo anti-cancer activities in animals and further apply it into clinical practices.